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Journal of Biomolecular Screening
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Practical Approaches to Efficient Screening: Information-Rich Screening Protocol

Prabha S. Karnachi, Ph.D.

Johnson & Johnson Pharmaceutical Research and Development, LLC 1000 Route 202, P.O. Box 300 Raritan, NJ 08869 pkarnach{at}prdus.jnj.com

Frank K. Brown

Johnson& Johnson Pharmaceutical Research and Development, LLC, Raritan, NJ.

The past approach of high-throughput screening of everything in the corporate collection has been shown to be very expensive in terms of reagents cost, disposal cost, and compound collection depletion. It is well known that screening campaigns produce several hits, ofwhich only 50% confirmon average. More efficientways of screening can provide an informative structure-activity relationship (SAR), which in turn can be used to buildmathematical models for further probing the activity space and directing chemical synthesis. The authors report new methods and insights to extract themaximum possible information from a screening experiment and findmost of the possible hits in the corporate collection while screening as few compounds as possible.

Key Words: iterative focused screening • in silico screening • sequential screening • cluster-based follow-up screening

Journal of Biomolecular Screening, Vol. 9, No. 8, 678-686 (2004)
DOI: 10.1177/1087057104269570
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